Anti-inflammatory and remyelinating effects of AZD4547 in experimental
multiple sclerosis
Abstract
Background and Purpose: Fibroblast Growth Factor (FGF), VEGFR2, and
CSF1R signalling pathways play a key role in the pathogenesis of
multiple sclerosis (MS). Selective inhibition of FGFR by infigratinib in
MOG35-55-induced EAE prevented severe first clinical episodes by 40%;
inflammation and neurodegeneration were reduced, and remyelination was
enhanced. Multi-kinase inhibition of FGFR1-3, CSF1R and VEGFR2 by
AZD4547 may be more efficient in reducing inflammation,
neurodegeneration and regeneration in the disease model. Experimental
Approach: Female C57BL/6J mice were treated with AZD4547 (6.25 mg kg-1
or 12.5 mg kg-1) orally or placebo over 10 days either from time of EAE
induction (prevention experiment) or onset of symptoms (suppression
experiment). Effects on inflammation, neurodegeneration and
remyelination were assessed at the peak of the disease (day 18/20 p.i.)
and the chronic phase of EAE (day 41/42 p.i.). Key Results: In the
prevention experiment, treatment with AZD4547 prevented severe first
clinical episodes by 66.7 or 84.6% respectively. Mice treated with 12.5
mg kg-1 of AZD4547 hardly showed any symptoms in the chronic phase of
EAE. In the suppression experiment, treatment with AZD4547 resulted in a
long-lasting reduction of severe symptoms by 91 or 100%. Inflammation
and demyelination were reduced, and axonal density, numbers of
oligodendrocytes and their precursor cells, and remyelinated axons were
increased in both experimental approaches. Conclusion and Implications:
Multi-kinase inhibition by AZD4547 in a well-tolerated dose of 1 mg kg-1
in humans may be a promising approach to reduce inflammation and
neurodegeneration, to slow down disease progression and support
remyelination in patients.